A facile synthesis of 6-[(4-nitrophenyl)thio]-substituted 2-methylene-2,3-dihydro-1,4-oxazepines from N-propargylic beta-enaminones
SYNTHETIC COMMUNICATIONS
Authors: Kelgokmen, Yilmaz; Korkmaz, Esra; Zora, Metin
Abstract
A one-pot process for the synthesis of 6-[(4-nitrophenyl)thio]-substituted 2-methylene-2,3-dihydro-1,4-oxazepines is reported. When reacted with 4-nitrobenzenesulfenyl chloride, N-propargylic beta-enaminones afforded alpha-sulfenylated N-propargylic beta-enaminones, which, in the presence of zinc chloride, underwent electrophilic cyclization to yield 6-[(4-nitrophenyl)thio]-substituted 2-methylene-2,3-dihydro-1,4-oxazepines. Process was found to be general for various N-propargylic beta-enaminones along with large substrate scope and high functional group tolerance. This operationally easy method may provide quick access to a library of functionalized 1,4-oxazepines of pharmacological interest.
Overview of the Nucleic-Acid Binding Properties of the HIV-1 Nucleocapsid Protein in Its Different Maturation States
VIRUSES-BASEL
Authors: Mouhand, Assia; Pasi, Marco; Catala, Marjorie; Zargarian, Loussine; Belfetmi, Anissa; Barraud, Pierre; Mauffret, Olivier; Tisne, Carine
Abstract
HIV-1 Gag polyprotein orchestrates the assembly of viral particles. Its C-terminus consists of the nucleocapsid (NC) domain that interacts with nucleic acids, and p1 and p6, two unstructured regions, p6 containing the motifs to bind ALIX, the cellular ESCRT factor TSG101 and the viral protein Vpr. The processing of Gag by the viral protease subsequently liberates NCp15 (NC-p1-p6), NCp9 (NC-p1) and NCp7, NCp7 displaying the optimal chaperone activity of nucleic acids. This review focuses on the nucleic acid binding properties of the NC domain in the different maturation states during the HIV-1 viral cycle.